PCSK9

Proprotein convertase subtilisin/kexin type 9

The protein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme encoded by the PCSK9 gene located on human chromosome 1. It is the ninth member of the protein convertase family, a group of enzymes that can activate homologous genes found in many species^[1]. PCSK9 is a liver-synthesized protease that plays a major role in regulating the levels of low-density lipoprotein receptors (LDLR) on the surface of liver cells and can inhibit the LDLR recycling pathway. PCSK9 binds to LDLR on the surface of liver cells, escorts LDLR to lysosomes for degradation, and prevents LDLR from recirculating to the cell membrane, effectively increasing the level of circulating LDL. Therefore, inhibiting the activity of the PCSK9 protease can down-regulate circulating LDL levels. PCSK9 is closely associated with various cardiovascular diseases, especially hypercholesterolemia and atherosclerosis^[2].

References:

[1]. Horton JD, et al. PCSK9: a convertase that coordinates LDL catabolism. J Lipid Res. 2009 Apr;50 Suppl(Suppl):S172-7. [Content Brief]

[2]. Peterson AS, et al. PCSK9 function and physiology. J Lipid Res. 2008 Jun;49(6):1152-6. [Content Brief]

PCSK9 Related Products (79):

By Effects:	Inhibitors (69) Degraders (2) Modulators (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-P99816

Ralpancizumab	Inhibitor
Ralpancizumab is a selective PCSK9 inhibitor with potential application in hemorrhagic stroke.

HY-147252

Bezeparsen	Inhibitor
Bezeparsen is a PCSK9 synthesis inhibitor.

HY-P990485

Anti-PCSK9 Antibody	Inhibitor
Anti-PCSK9 Antibody is a human antibody expressed in CHO, targeting PCSK9. Anti-PCSK9 Antibody contains a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-PCSK9 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

HY-128334

PCSK9 modulator-2	Modulator
PCSK9 modulator-2 (Compound 1) is a potent modulator of PCSK9 with an EC₅₀ value of 202 nM. PCSK9 is a recently validated target for lowering low-density lipoprotein cholesterol (LDL-C). PCSK9 modulator-2 has the potential for the research of hyperlipidemia.

HY-153452

PCSK9-IN-16	Inhibitor
PCSK9-IN-16 is a potent PCSK9 inhibitor. PCSK9-IN-16 is extracted from patent WO2020150474, example 87, has the potential for hypercholesterolemia and other cardiovascular diseases research.

HY-155006

PCSK9-IN-19	Inhibitor
PCSK9-IN-19 (Compound 1) is a PCSK9 inhibitor. PCSK9-IN-19 can be used for research of high LDL-cholesterol levels and prevention of coronary artery disease.

HY-148689

SPC4061	Inhibitor
SPC4061 an antisense nucleotide, is a potent PCSK9 inhibitor. SPC4061 targets the lock-in nucleic acid (LNA) of PCSK9 for the study of hypercholesterolemia and related diseases.

HY-141724

PCSK9 ligand 1	Inhibitor
PCSK9 ligand 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) ligand. PCSK9 ligand 1 does not affect PCSK9 function.

HY-146084

PCSK9 modulator-3	Modulator
PCSK9 modulator-3 (Compound 13) is a potent modulator of PCSK9 with an EC₅₀ value of 2.46 nM. PCSK9 is a recently validated target for lowering low-density lipoprotein cholesterol (LDL-C). PCSK9 modulator-3 has the potential for the research of hyperlipidemia.

HY-130245A

(R,R)-PCSK9 degrader 1	Degrader
(R,R)-PCSK9 degrader 1 is the isomer of PCSK9 degrader 1 (HY-130245). PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a K_i of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor.

HY-153454

PCSK9-IN-18	Inhibitor
PCSK9-IN-18 (compound 188) is a potent PCSK9 inhibitor with a K_D value of <200 nM.

HY-160036

PCSK9-IN-22	Inhibitor
PCSK9-IN-22 (compound 29) is an orally active inhibitor of PCSK9. PCSK9-IN-22 inhibits the interaction of the protein with LDLR in vivo.

HY-161434

PCSK9-IN-26	Inhibitor
PCSK9-IN-26 (Compound 116) is an PCSK9 inhibitor (IC₅₀ < 1 nM). PCSK9-IN-26 can be used for metabolic research.

HY-161942

PCSK9-IN-31	Inhibitor
PCSK9-IN-31 (Compound WX002) is an orally active PCSK9 inhibitor. PCSK9-IN-31 can lower low-density lipoprotein cholesterol (LDL-C) and total cholesterol (TC) in high cholesterol fed model rats.

HY-153391

PCSK9-IN-14	Inhibitor
PCSK9-IN-14 (compound Ia-8) is a potent PCSK9 inhibitor.

HY-161435

PCSK9-IN-27	Inhibitor
PCSK9-IN-27 (Compound 108) is a PCSK9 inhibitor (IC₅₀: 3.4 nM). PCSK9-IN-27 reduces LDLR degradation and increases LDL-C uptake.

HY-147252A

Bezeparsen sodium	Inhibitor
Bezeparsen sodium is a PCSK9 synthesis inhibitor.

HY-P99552

Tafolecimab	Inhibitor
Tafolecimab (IBI-306) is a human lgG2 monoclonal antibody that specifically binds PCSK-9 and reduces LDL-C levels by inhibiting PCSK-9-mediated endocytosis of the LDL receptor, which in turn enhances clearance of LDL-C and leads to a reduction in LDL-C levels. Tafolecimab may be used in studies of hypercholesterolaemia.

HY-153453

PCSK9-IN-17	Inhibitor
PCSK9-IN-17 is a PCSK9 inhibitor. PCSK9-IN-17 can be used for the research of cholesterol metabolism (WO2020150474A1, compound 105).

HY-163141

PCSK9-IN-24	Inhibitor
PCSK9-IN-24 (Compound OY3) is a compound that targets PCSK9. PCSK9-IN-24 reduces PCSK9 levels and increases LDL uptake and may be used in atherosclerosis research.

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